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J Biol Chem, Vol. 273, Issue 46, 30316-30320, November 13, 1998
,
From the The broad spectrum antibacterial properties of
2-hydroxydiphenyl ethers have been appreciated for decades, and their
use in consumer products is rapidly increasing. We identify the
enoyl-acyl carrier protein reductase (fabI) component of
the type II fatty acid synthase system as the specific cellular target
for these antibacterials. Biologically active 2-hydroxydiphenyl ethers
effectively inhibit fatty acid synthesis in vivo and FabI
activity in vitro. Resistant mechanisms include
up-regulation of fabI expression and spontaneously arising
missense mutations in the fabI gene. These results
contradict the view that these compounds directly disrupt membranes and
suggest that their widespread use will select for resistant bacterial populations.
Department of Biochemistry, St. Jude
Children's Research Hospital, Memphis, Tennessee 38105, the
§ Department of Molecular Biology and ¶ Department of
Infectious Diseases, Parke-Davis Pharmaceutical Research, Ann Arbor,
Michigan 48105, and the Department of Biochemistry, University
of Tennessee, Memphis, Tennessee 38163
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